Guo Lu-Lu, Zhang Chen, Huang Yan-Jun, Liu Xing-Yu, Liu De-Shui, Long Teng, Sun Jin-Hao, Liu Shao-Feng, Li Zhong-Hao, Wang Jia-Zhong, Mao Jian
Beijing Life Science Academy Co., Ltd., Beijing 102209, China.
Department of Nutrition and Health, China Agricultural University, Beijing 100193, China.
Se Pu. 2025 Apr 8;43(4):363-371. doi: 10.3724/SP.J.1123.2024.10005.
Nicotine, the principal alkaloid in tobacco, exhibits significant central nervous system activity and induces a wide array of physiological effects. In addition to its well-documented role in tobacco dependence, previous studies have suggested that nicotine also has diverse pharmacological properties. These include alleviating symptoms associated with Parkinson's disease, potentially reducing the risk of Alzheimer's disease, mitigating oxidative stress, as well as anti-inflammatory and anxiolytic effects. Neuroscientists frequently use an array of molecular biology techniques to elucidate the mechanisms responsible for the effects of nicotine on the central nervous system. However, disease onset is invariably accompanied by metabolic dysfunction, and organisms often exhibit complex and unpredictable responses to pharmacological stimuli. As a bioactive alkaloid with potent pharmacological properties, nicotine is able to cross the blood-brain barrier and induce brain-compound changes, which serves as the basis for its effects on the central nervous system. Consequently, examining the extensive impact of nicotine exposure on endogenous metabolites and metabolic pathways in the brain is an indispensable step toward providing a more robust foundation for understanding the complex physiological effects of nicotine. In this study, an ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) metabolomic-analysis method was established to systematically examine the effects of repeated nicotine exposure on endogenous metabolites in mouse brains. Two chromatographic systems fitted with Acquity UPLC BEH HILIC (150 mm×2.1 mm, 1.7 μm) and BEH C18 (150 mm×2.1 mm, 1.7 μm) columns were used to determine the nicotine present in samples. As a result, the established UHPLC-MS/MS method identified a total of 759 endogenous metabolites. Compared with the saline group, nicotine exposure resulted in 575 significantly different metabolites, with 434 metabolites down-regulated and 141 up-regulated. Further pathway-enrichment analysis using the Kyoto Encyclopedia of Genes and Genomes (KEGG) revealed that nicotine exposure primarily affects essential-amino-acid, lipid, nucleotide, carbohydrate, cofactor, and vitamin metabolism, as well as other amino-acid metabolic pathways in the brain. Although non-targeted metabolomics can simultaneously detect and analyze all small-molecule metabolites in an unbiased manner, accurately capturing metabolite changes in specific brain regions is challenging when dealing with complex brain-tissue systems. Targeting the aggregation of material bases and the delivery of precision treatment to certain brain regions is expected to be significant for the targeted therapy of central nervous system diseases. Airflow-assisted desorption electrospray ionization mass spectrometry imaging (AFADESI-MSI) was further used to directly visualize the nicotine-induced distributions and variations of differentially expressed metabolites in various brain regions, which revealed that nicotine exposure leads to the significant downregulation of choline, serine, aspartate, and malate levels throughout the brain. Specifically, taurine, acetylcholine, and adenosine levels were notably affected in the cortical, hippocampal, and striatal regions, respectively. Essential-amino-acid metabolism was most affected by nicotine, with lipid metabolism found to be the next-most affected pathway. These metabolic pathways predominantly affected the cortical region, whereas the striatum, hippocampus, thalamus, and cerebellum were affected to varying degrees. These findings provide novel experimental evidence that enhances our understanding of metabolic biomarkers associated with nicotine exposure.
尼古丁是烟草中的主要生物碱,具有显著的中枢神经系统活性,并能引发一系列生理效应。除了在烟草依赖中广为人知的作用外,先前的研究表明尼古丁还具有多种药理特性。这些特性包括缓解与帕金森病相关的症状、可能降低患阿尔茨海默病的风险、减轻氧化应激以及具有抗炎和抗焦虑作用。神经科学家经常使用一系列分子生物学技术来阐明尼古丁对中枢神经系统产生作用的机制。然而,疾病的发生总是伴随着代谢功能障碍,生物体对药理刺激往往会表现出复杂且不可预测的反应。作为一种具有强大药理特性的生物活性生物碱,尼古丁能够穿过血脑屏障并引起脑内化合物变化,这是其对中枢神经系统产生作用的基础。因此,研究尼古丁暴露对脑内内源性代谢物和代谢途径的广泛影响,是为理解尼古丁复杂的生理效应提供更坚实基础的不可或缺的一步。在本研究中,建立了一种超高效液相色谱 - 串联质谱(UHPLC-MS/MS)代谢组学分析方法,以系统地研究重复尼古丁暴露对小鼠脑内内源性代谢物的影响。使用配备了Acquity UPLC BEH HILIC(150 mm×2.1 mm,1.7 μm)和BEH C18(150 mm×2.1 mm,1.7 μm)色谱柱的两个色谱系统来测定样品中的尼古丁。结果,所建立的UHPLC-MS/MS方法共鉴定出759种内源性代谢物。与生理盐水组相比,尼古丁暴露导致575种代谢物存在显著差异,其中434种代谢物下调,141种上调。使用京都基因与基因组百科全书(KEGG)进行的进一步通路富集分析表明,尼古丁暴露主要影响脑内必需氨基酸、脂质、核苷酸、碳水化合物、辅因子和维生素代谢,以及其他氨基酸代谢途径。尽管非靶向代谢组学可以无偏向地同时检测和分析所有小分子代谢物,但在处理复杂的脑组织系统时,准确捕获特定脑区的代谢物变化具有挑战性。针对某些脑区的物质基础聚集和精准治疗递送进行靶向研究,有望对中枢神经系统疾病的靶向治疗具有重要意义。气流辅助解吸电喷雾电离质谱成像(AFADESI-MSI)进一步用于直接可视化尼古丁诱导的各种脑区内差异表达代谢物的分布和变化,结果显示尼古丁暴露导致全脑胆碱、丝氨酸、天冬氨酸和苹果酸水平显著下调。具体而言,牛磺酸、乙酰胆碱和腺苷水平分别在皮质、海马和纹状体区域受到显著影响。必需氨基酸代谢受尼古丁影响最大,脂质代谢是其次受影响最大的途径。这些代谢途径主要影响皮质区域,而纹状体、海马、丘脑和小脑也受到不同程度的影响。这些发现提供了新的实验证据,增强了我们对与尼古丁暴露相关的代谢生物标志物的理解。